Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one.

Swagatika Das, Praveen K Roayapalley, Sarvesh C Vashishtha, Umashankar Das, Jonathan R Dimmock
{"title":"Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one.","authors":"Swagatika Das,&nbsp;Praveen K Roayapalley,&nbsp;Sarvesh C Vashishtha,&nbsp;Umashankar Das,&nbsp;Jonathan R Dimmock","doi":"10.3390/medicines10090054","DOIUrl":null,"url":null,"abstract":"<p><p>There is a need for novel antiepileptic agents whose modes of action differ from those of current antiepileptic drugs. The objective of this study was to determine whether 1-diethylamino-3-phenylprop-2-en-1-one (<b>2</b>) could prevent or at least diminish convulsions caused by different mechanisms. This amide afforded protection in the maximal electroshock and subcutaneous pentylenetetrazole screens when given intraperitoneally to both mice and rats. A number of specialized tests in mice were conducted and are explained in the text. They revealed (<b>2</b>) to have efficacy in the 6 Hz psychomotor seizure test, the corneal kindling model, the mouse temporal epilepsy screen and a peripheral neuronal transmission test using formalin. Three screens in rats were undertaken, which revealed that (<b>2</b>) blocked chloride channels, inhibited peripheral neuronal transmission (tested using sciatic ligation and von Frey fibres) and afforded protection in the lamotrigine-resistant kindled rat model. The biodata generated reveal that (<b>2</b>) is an important lead molecule in the quest for novel structures to combat epilepsy.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2023-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10535378/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicines (Basel, Switzerland)","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3390/medicines10090054","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

Abstract

There is a need for novel antiepileptic agents whose modes of action differ from those of current antiepileptic drugs. The objective of this study was to determine whether 1-diethylamino-3-phenylprop-2-en-1-one (2) could prevent or at least diminish convulsions caused by different mechanisms. This amide afforded protection in the maximal electroshock and subcutaneous pentylenetetrazole screens when given intraperitoneally to both mice and rats. A number of specialized tests in mice were conducted and are explained in the text. They revealed (2) to have efficacy in the 6 Hz psychomotor seizure test, the corneal kindling model, the mouse temporal epilepsy screen and a peripheral neuronal transmission test using formalin. Three screens in rats were undertaken, which revealed that (2) blocked chloride channels, inhibited peripheral neuronal transmission (tested using sciatic ligation and von Frey fibres) and afforded protection in the lamotrigine-resistant kindled rat model. The biodata generated reveal that (2) is an important lead molecule in the quest for novel structures to combat epilepsy.

Abstract Image

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
1-二乙氨基-3-苯基丙-2-烯-1-酮的抗惊厥性能。
需要新的抗癫痫药物,其作用模式不同于目前的抗癫痫药。本研究的目的是确定1-二乙氨基-3-苯基丙-2-烯-1-酮(2)是否可以预防或至少减轻由不同机制引起的抽搐。当腹膜内给予小鼠和大鼠时,这种酰胺在最大电击和皮下戊四唑屏蔽中提供保护。在小鼠身上进行了一些专门的测试,并在文本中进行了解释。他们发现(2)在6赫兹精神运动性癫痫测试、角膜点燃模型、小鼠颞叶癫痫筛查和使用福尔马林的外周神经元传递测试中具有疗效。在大鼠中进行了三次筛选,结果显示:(2)阻断氯通道,抑制外周神经元传递(使用坐骨神经结扎和von Frey纤维进行测试),并在拉莫三嗪抗性点燃大鼠模型中提供保护。产生的生物数据表明,(2)是寻找新型结构来对抗癫痫的重要先导分子。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 去求助
来源期刊
自引率
0.00%
发文量
0
审稿时长
6 weeks
期刊最新文献
Breathing for Two: Asthma Management, Treatment, and Safety of Pharmacological Therapy during Pregnancy. GDF15 Targeting for Treatment of Hyperemesis Gravidarum. Deciphering Mechanisms, Prevention Strategies, Management Plans, Medications, and Research Techniques for Strokes in Systemic Lupus Erythematosus. Cytokine Storm in COVID-19: Insight into Pathological Mechanisms and Therapeutic Benefits of Chinese Herbal Medicines. Incidence and Outcomes of COVID-19 Vaccine Hypersensitivity Reactions and Success of COVID-19 Vaccine Provocation Tests Post Previous COVID-19 Vaccine Hypersensitivity.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1